Tirzepatide
An approved dual GIP and GLP-1 receptor agonist peptide for type 2 diabetes and obesity, given by once-weekly injection.
Overview
Tirzepatide is a synthetic peptide that acts as an agonist at both the GIP and GLP-1 receptors, the first dual incretin agonist to reach approval (Mounjaro for type 2 diabetes and Zepbound for obesity). It is administered by once-weekly subcutaneous injection and has produced some of the largest mean weight losses seen in obesity pharmacotherapy trials.
Mechanism
Tirzepatide is engineered as a single peptide with activity at both receptors. The GIP component is believed to augment the GLP-1-mediated effects on appetite and insulin secretion, although the exact contribution of GIP agonism is still being defined. Net effects include glucose-dependent insulin release, reduced food intake, and improved insulin sensitivity.
Dosing
Approved use is once-weekly subcutaneous injection with dose titration over several weeks to the maintenance dose. Doses are label-defined, and use outside prescribing is not clinically validated.
- Weekly subcutaneous dosing per the approved labels
- Gradual titration reduces gastrointestinal intolerance
- Research-context use outside approved indications is unsupported
Expected Effects
- Large reductions in HbA1c in type 2 diabetes trials
- Substantial dose-dependent weight loss in obesity trials
- Improvements in lipids and blood pressure reported in trials
Side Effects & Tolerability
Gastrointestinal events, including nausea, diarrhea, vomiting, and constipation, are the most common adverse effects. Label warnings cover pancreatitis, gallbladder disease, and thyroid C-cell tumors observed in rodents. As a relatively new drug, long-term safety continues to be monitored.
Storage
Approved products are stored refrigerated before first use. Lyophilized research peptide should be stored cold and desiccated, protected from light, per the supplier certificate of analysis.